1. Field of the Invention
The present invention relates to an ibuprofen-containing antipyretic analgesic preparation, and more specifically, it relates to an ibuprofen-containing antipyretic analgesic preparation comprising ibuprofen, acetaminophen and magnesium-based antacids and/or a specific sedative.
2. Description of the Related Art
Numerous antipyretic analgesics are known in the prior art. Examples of those drugs that are widely used include combinations of aniline derivatives such as acetaminophen with salicylic acid derivatives such as aspirin and etoxybenzamide. However antipyretic analgesic preparations of salicylic acid derivatives have the disadvantage of easily causing gastric disorders. Thus, efforts are being made to develop antipyretic analgesic preparations having excellent efficacy and minimal acute toxicity by combining ibuprofen and antipyretic analgesic preparations of aniline derivatives in place of antipyretic analgesic preparations of salicylic acid derivatives (e.g., Japanese Unexamined Patent Publication Nos. 56-97224, 56-154416 and 59-104315).
Ibuprofen demonstrates superior antipyretic, analgesic and anti-inflammatory effects, and is widely used as a non-steroidal drug. However, in the case of oral administration of ibuprofen as well, there are cases of occurrence of feeling of discomfort in the stomach, gastralgia, nausea and so forth in the same manner as antipyretic analgesic preparations of salicylic acid derivatives, and the occurrence of gastric disorders has been indicated as a side effect of such preparations.
Consequently, combining the use of these preparations with salicylic acid derivatives (e.g., Japanese Unexamined Patent Publication No. 61-134315) or antacids and/or mucosal protective agents (e.g., Japanese Unexamined Patent Publication No. 63-198620) has been proposed for the purpose of relieving gastric disorders caused by oral administration of ibuprofen. However, the antipyretic analgesic preparations containing the drugs mentioned above were not always able to satisfy both antipyretic analgesic effects and relief of gastric disorders.
As stated above, although antacids are important ingredients that suppress the side effects of ibuprofen, the manufacturing of preparations of ibuprofen and antacids is difficult due to the occurrence of remarkable changes by the combination. Generally, in the case of pharmaceutical manufacturing preparations of ingredients in which compatibility changes occur, a method is used wherein layered tablets, press-coated tablets and each ingredient are coated with saccharide or polymer films (Japanese Unexamined Patent Publication No. 2-286614). However, in the case of simply layering or press-coat blending of ibuprofen, antacids and acetaminophen, there are disadvantages including being unable to prevent coloring and fusion of each ingredient at the interfaces, reduced content of ibuprofen, and unpleasant odor and taste.
In addition, manufacturing methods wherein ibuprofen, antacids and acetaminophen are separately coated with saccharides or polymer films require considerable processing time and are expensive due to the need for raw materials for the coating agent. Moreover, these methods also have the disadvantages of disintegration and elution of each ingredient due to the coating, along with incomplete separation of each ingredient due to partial destruction of the coating due to compression molding (tableting) in the case of tablet production.
On the other hand, examples of methods known in the prior art for prolonging the effects of drugs include:
(1) Methods which extend the disintegration properties of the preparation in the form of lozenges, pills and so forth;
(2) Methods which form multi-layer coated tablets by sugar coating the outside layer of the tablet and applying an enteric coating to the inside layer by means of a film coating;
(3) Methods which form spansule capsules in which capsules are filled with granules having different disintegration times;
(4) Methods which form span tab types in which granules having different disintegration times are formed into tablets;
(5) Methods which form spantabs, multi-layered spantabs in which fast-releasing granules and slow-releasing granules are divided and formed into tablets with two or three layers; and,
(6) Methods which form tablets in which the release of medication is controlled by a polymer matrix. However, although these prolonged-action pharmaceuticals are improved in terms of increased duration of the medication, they also have disadvantages including (1) insufficient fast-acting properties, (2) a complex manufacturing process, and (3) difficulties in stabilization of ingredients.